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MP470
Under development by SuperGen, MP470 inhibits not only wild-type c-Kit, but also imatinib-resistant mutants including V560G, D816V, N822K and K642E. It also inhibits AXL kinase and cMet, which are upregulated in some imatinib-resistant GISTs. Finally, it also inhibits Rad51 protein. An exciting paper about preclinical work with MP470 appeared in February 2007 (click here for abstract).
Link Here for additional information at the SuperGen website.
SuperGen announced July 5, 2007 the opening of the first Phase I trial for MP470 in Scottsdale, Arizona and in San Antonio, Texas. According to the announcement: "The trial is expected to enroll up to 30 patients at the two study centers. The Phase I trial is an accelerated titration dose-escalation study designed to assess the safety and tolerability of MP470, and to determine the maximum tolerated dose of the compound in patients with advanced-stage solid tumors. Additionally, the Company will assess pharmacokinetic and biomarker data from the study to assist in designing follow-on clinical studies for the use of MP470 as a single agent and in combination treatment modalities."
The Phase I trial description is shown at clinicaltrials.gov
